PROTAC NTRK1 degrader-1
PROTAC NTRK1 degrader-1 is a wild-type and mutant NTRK1 PROTAC degrader with IC50 values of 4 nM (wild-type), 2 nM (G595R), 5 nM (G667C), and <0.5 nM (F598L). PROTAC NTRK1 degrader-1 catalyzes ubiquitination and subsequent proteasome-mediated degradation of wild-type and mutant (G595R, G667C, F598L) NTRK1. PROTAC NTRK1 degrader-1 can be used for the research of solid tumors.
(Pink: NTRK1 ligand (HY-185545); Blue: Cereblon ligand (HY-W1115186); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 2922274-35-7
- Formula: C38H35FN10O6
- Molecular Weight:746.75
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
In Vitro
NTRK degrader-1 (compound 5b) (6 h) degrades wild-type NTRK1, NTRK1G595R, NTRK1G667C, and NTRK1F598L in 293 T cells at 6 h, with the IP (inflection point) values of 0.2 nM, 1 nM, 2 nM, and 0.2 nM, respectively[1].
NTRK degrader-1 inhibits wild-type NTRK1, NTRK1G595R, NTRK1G667C, and NTRK1F598L with IC50 values of 4 nM, 2 nM, 5 nM and <0.5 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | CL | T1/2 | Vss |
|---|---|---|---|---|---|
| Mice[1] | 0.5 mg/kg | i.v. | 62 mL/mg/kg | 1.6 h | 3.1 L/kg |
Chemical Information
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CAS No. 2922274-35-7
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Molecular Weight 746.75
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Formula C38H35FN10O6
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SMILES
O=C1NC(C=CC(C(NCC(N2CCN(C3=CC=C(NC4CCC(NC4=O)=O)C=C3)CC2)=O)=O)=C5)=C5OC(C=CC(F)=C6)=C6CNC7=NC8=C1C=NN8C=C7
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC NTRK1 degrader-1 Related Classifications
HY-181052 Related Classifications
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